Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/405)
  • Patent number: 10196374
    Abstract: This specification generally relates to 1-alkyl-6-oxo-1,6-dihydropyridin-3-yl compounds (including salts thereof). This specification also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including treatment methods and medicament preparations), and processes for making such a compound.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: February 5, 2019
    Assignee: AstraZeneca AB
    Inventors: Lena Elisabeth Ripa, Karolina Lawitz, Matti Juhani Lepistö, Martin Hemmerling, Karl Edman, Antonio LLinas
  • Patent number: 10189809
    Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: January 29, 2019
    Assignee: Ironwood Pharmaceuticals, Inc.
    Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R. Iyengar, Ara Mermerian, Angelika Fretzen
  • Patent number: 10047082
    Abstract: The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: August 14, 2018
    Assignee: Corcept Therapeutics, Inc.
    Inventors: Hazel Hunt, Iain Walters, Benoit Gourdet
  • Patent number: 9550763
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect, e.g. a compound of Formula (I): wherein R2 is a hydrogen atom or the like; ring A is five- to seven-cycloalkane or the like; C is a carbon atom; Q1 and Q2 are carbon atoms or the like; R9a and R9b are carbon atoms or the like; R6 is cycloalkyl or the like; R7 is a group represented by the formula: wherein ring D is benzene or the like; carbon atom a and b are carbon atoms; ring B is an aromatic carbocyclic ring or the like; s and s? are 0 or the like; R9 and R9? are halogen or the like, or the like, or its pharmaceutically acceptable salt.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: January 24, 2017
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Hiroyuki Kai, Satoru Tanaka, Yoshiharu Hiramatsu, Azusa Nozu, Ken'ichioh Nakamura
  • Patent number: 9518182
    Abstract: There is described a polysiloxane having the structure: wherein R1, R2, and R3 are independently a hydrocarbon radical, an unsaturated radical, an alkoxy radical, an aryl radical or an alkenyloxy radical, R4 is independently a direct bond or hydrocarbon radical optionally substituted with oxygen and nitrogen, R5 is independently a hydrogen, a halogen, an aliphatic group having from 1 to 6 carbon atoms, an aromatic group having 6 to 8 carbon atoms, an alkoxy group having from 1 to 6 carbon atoms, or an aryloxy group, R6 is independently a hydroxyl group, an amine group, an acid chloride group, or a sulfonyl halide group, x is from 1 to 300; y is from 0 to 50; and z is from 0 to 50. The polysiloxane is used to make various copolymers and polymer blends. A variety of articles can be made using the polysiloxane described as a polymer blend or copolymer.
    Type: Grant
    Filed: July 2, 2015
    Date of Patent: December 13, 2016
    Assignee: Momentive Performance Materials, Inc.
    Inventors: Narayana Padmanabha Iyer, Indumathi Ramakrishnan, Anuj Mittal, Roy Rojas-Wahl, Samim Alam
  • Patent number: 9309235
    Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: April 12, 2016
    Assignee: IRONWOOD PHARMACEUTICALS, INC.
    Inventors: G-Yoon Jamie Im, Rajesh Iyengar, Joel Moore, Angelika Fretzen
  • Patent number: 9282743
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides and herbicides.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: March 15, 2016
    Assignee: Syngenta Participations AG
    Inventors: Tomas Smejkal, Michel Muehlebach
  • Patent number: 9012441
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: April 21, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Patent number: 9006258
    Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: April 14, 2015
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Allen A. Fienberg, Sharon Mates, Lawrence P. Wennogle
  • Publication number: 20150072986
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Application
    Filed: June 11, 2014
    Publication date: March 12, 2015
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim, Minh Ngoc Nguyen, Elizabeth Enlow
  • Patent number: 8865758
    Abstract: The present invention is related to pyrazolo piperidine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: October 21, 2014
    Assignee: Genkyotex SA
    Inventors: Patrick Page, Benoît Laleu, Francesca Gaggini, Mike Orchard
  • Patent number: 8841337
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: September 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Pierre-Henri Storck, Joanne Pinder, John R. Studley
  • Patent number: 8815871
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: August 26, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • Patent number: 8809329
    Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: August 19, 2014
    Assignees: Tokyo Metropolitan Institute of Medical Science, Renascience Co., Ltd.
    Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
  • Patent number: 8802711
    Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof, wherein X1, X2, X3, X4, J, K, L, X5, X6, Rb, G2, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: August 12, 2014
    Assignee: AbbVie Inc.
    Inventors: Arthur Gomtsyan, Jerome F. Daanen, Gregory A. Gfesser, Michael E. Kort, Chih-Hung Lee, Heath A. McDonald, Pamela S. Puttfarcken, Eric A. Voight, Philip R. Kym
  • Patent number: 8802712
    Abstract: The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: August 12, 2014
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Werner Mederski, Frank Zenke
  • Publication number: 20140148339
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides and herbicides.
    Type: Application
    Filed: June 22, 2012
    Publication date: May 29, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Tomas Smejkal, Michel Muehlebach
  • Patent number: 8697737
    Abstract: The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: April 15, 2014
    Assignee: Exelixis, Inc.
    Inventors: Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Larisa Dubenko, Abigail R. Kennedy, Steven Charles Defina, Angie I. Kim, Jean-Claire L. Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Anagha Abhijit Joshi
  • Patent number: 8680081
    Abstract: The present invention provides methods and compositions for the prophylactic or targeted prophylactic treatment of migraine. In one embodiment a patient is regularly given a therapeutically effective amount of a combination of a cyclooxygenase-2 inhibitor and acetylsalicylic acid or active derivative, for prophylactic treatment of migraine. In another embodiment, a patient, at a time prior to a determined time window, is administered a therapeutically effective amount of a cyclooxygenase-2 inhibitor, either alone or in combination with acetylsalicylic acid or active derivative, to prevent or reduce migraine symptoms during the time window. Representative compositions include a cyclooxygenase-2 inhibitor and acetylsalicylic acid or salicylate salt.
    Type: Grant
    Filed: August 27, 2001
    Date of Patent: March 25, 2014
    Inventor: Peter Van Patten
  • Patent number: 8648069
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: February 11, 2014
    Assignee: AbbVie Inc.
    Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn George, Lu Wang, Biqin Li, N. St. John Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
  • Patent number: 8623901
    Abstract: The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and R1 is the group V?W?*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: January 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Riccardo Giovannini, Cornelia Dorner-Ciossek, Christian Eickmeier, Dennis Fiegen, Thomas Fox, Klaus Fuchs, Niklas Heine, Holger Rosenbrock, Gerhard Schaenzle
  • Publication number: 20130344031
    Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
    Type: Application
    Filed: August 27, 2013
    Publication date: December 26, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
  • Publication number: 20130345270
    Abstract: Active compounds useful for inhibiting fatty acid synthase in a subject in need thereof are described. The active compounds are, in general, a 5-mercapto-1H-Indazole-4,7-dione or an analog thereof. The compounds are useful for treating subjects afflicted with, cancer, obesity, diabetes, a viral infection, a bacterial infection, a fungal infection, or a protozoal infection.
    Type: Application
    Filed: November 7, 2011
    Publication date: December 26, 2013
    Applicant: Waake Forest University Health Sciences
    Inventors: Steven J. Kridel, W. Todd Lowther, Herman W. Odens, Jeffrey D. Schmitt
  • Patent number: 8609649
    Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: December 17, 2013
    Assignee: Brandeis University
    Inventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R. P. Novak
  • Patent number: 8569302
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: October 29, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Mertzman, Philip A. Morganelli, William J. Watkins, Hong Ye
  • Patent number: 8557857
    Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
    Type: Grant
    Filed: July 29, 2008
    Date of Patent: October 15, 2013
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
  • Patent number: 8524751
    Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: September 3, 2013
    Assignee: GlaxoSmithKline Intellecutual Property Development
    Inventors: Julie Nicole Hamblin, Zoe Alicia Harrison, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Nigel James Parr
  • Patent number: 8481579
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: July 9, 2013
    Assignee: Chemocentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M. K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
  • Patent number: 8481533
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: July 9, 2013
    Assignee: University Health Network
    Inventors: Peter B. Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Radoslaw Laufer, Guohua Pan
  • Patent number: 8461194
    Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: June 11, 2013
    Assignee: Aziende Chimiche Riunite Angelini Francesco A. C. R. A. F. S. p. A.
    Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
  • Patent number: 8440691
    Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: May 14, 2013
    Assignee: AbbVie Inc.
    Inventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, Jr., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
  • Patent number: 8383662
    Abstract: Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: February 26, 2013
    Assignees: National Chiao Tung University, National Taiwan University
    Inventors: Chung-Ming Sun, Min-Liang Kuo, Yufeng Jane Tseng
  • Patent number: 8334322
    Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt of amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: December 18, 2012
    Assignee: Pisgah Laboratories, LLC
    Inventors: David William Bristol, Clifford Riley King, Joseph Pike Mitchener, Jr., Vicki Haynes Audia
  • Publication number: 20120277248
    Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.
    Type: Application
    Filed: June 13, 2012
    Publication date: November 1, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Michele CARUSO, Italo BERIA, Maria Gabriella BRASCA, Ron FERGUSON, Helena POSTERI
  • Patent number: 8263596
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: September 11, 2012
    Assignee: University Health Network
    Inventors: Peter B. Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Radoslaw Laufer
  • Patent number: 8252945
    Abstract: As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: August 28, 2012
    Assignees: UBE Industries, Ltd., Santen Pharmaceutical Co., Ltd.
    Inventors: Hisayuki Seike, Takeshi Matsugi, Atsushi Shimazaki
  • Patent number: 8236337
    Abstract: The presently disclosed and claimed invention is directed to anti-microbial orthodontic apparatus and anti-microbial orthodontic compositions comprising an effective amount of a selenium compound, kits containing same, and methods of producing and using said anti-microbial orthodontic apparatus and anti-microbial orthodontic compositions.
    Type: Grant
    Filed: July 13, 2009
    Date of Patent: August 7, 2012
    Assignee: Selenium, Ltd.
    Inventors: Ted Reid, Julian Spallholz, Thirumal N. Devanathan, Thomas Mosley
  • Publication number: 20120157465
    Abstract: A number of DNA methylation inhibitors are described. The DNA methylation inhibitors were identified using a two-component enhanced green fluorescent protein reporter system to screen a compound library containing procainamide derivatives. The DNA methylation inhibitors can be used for cancer therapy and prevention.
    Type: Application
    Filed: December 19, 2011
    Publication date: June 21, 2012
    Applicant: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Arthur Y. Shaw, Yu-Wei Leu, Shu-Huei Hsiao
  • Publication number: 20120129833
    Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system.
    Type: Application
    Filed: August 19, 2011
    Publication date: May 24, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ningshu LIU, Kai Thede, Philip Lienau, Arne Scholz, Maher Najjar, Ulf Bomer, Knut Eis, Reiner Fischer
  • Publication number: 20120108584
    Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.
    Type: Application
    Filed: January 11, 2012
    Publication date: May 3, 2012
    Applicant: SANOFI-AVENTIS
    Inventors: Laurent DUBOIS, Yannick Evanno, Christian Maloizel, Mireille Sevrin
  • Patent number: 8163743
    Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: April 24, 2012
    Assignee: GlaxoGroupLimited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Christian Alan Paul Smethurst, Yoshiaki Washio
  • Publication number: 20120071503
    Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.
    Type: Application
    Filed: March 18, 2011
    Publication date: March 22, 2012
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Nicholas D. P. Cosford, Dhanya Raveendra Panickar, Shyama Sidique
  • Publication number: 20120040963
    Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.
    Type: Application
    Filed: January 31, 2011
    Publication date: February 16, 2012
    Applicant: Bayer CropScience AG
    Inventors: Reiner FISCHER, Thomas BRETSCHNEIDER, Ernst Rudolf F. GESING, Dieter FEUCHT, Karl-Heinz KUCK, Peter LÖSEL, Olga MALSAM, Christian ARNOLD, Thomas AULER, Martin Jeffrey HILLS, Heinz KEHNE
  • Patent number: 8101644
    Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: January 24, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
  • Patent number: 8084485
    Abstract: 6-(Aminoalkyl)indazoles of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, and renal, cardiac and vascular protecting medicinally active ingredients.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: December 27, 2011
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
  • Patent number: 8067457
    Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.
    Type: Grant
    Filed: October 26, 2006
    Date of Patent: November 29, 2011
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
  • Publication number: 20110288088
    Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.
    Type: Application
    Filed: May 17, 2011
    Publication date: November 24, 2011
    Applicant: NERVIANO MEDICAL SCIENCES S.r.I.
    Inventors: Tiziano BANDIERA, Andrea LOMBARDI BORGIA, Sten Christian ORRENIUS, Ettore PERRONE, Italo BERIA, Daniele FANCELLI, Arturo GALVANI
  • Patent number: 8063091
    Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: November 22, 2011
    Assignee: Abbott Laboratories
    Inventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
  • Patent number: 8053459
    Abstract: The present invention synthesizes a series of selenolo[3,2-c]pyrazole and selenolo[2,3-c]pyrazole derivatives, and discovers their anticancer activity.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: November 8, 2011
    Assignee: China Medical University
    Inventors: Sheng-Chu Kuo, Li-Jiau Huang, Li-Chen Chou, Jai-Sing Yang, Mei-Hua Hsu, Shi-Hong Zhuang, Mei-Chi Fang, Hui-Yi Lin
  • Publication number: 20110263598
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Application
    Filed: April 6, 2011
    Publication date: October 27, 2011
    Applicant: UNIVERSITY HEALTH NETWORKS
    Inventors: Peter B. Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Radoslaw Laufer, Guohua Pan